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Lipid based nanoparticles: drug delivery platform
Voldřichová, Lenka ; Holas, Ondřej (advisor) ; Svačinová, Petra (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Supervisor: PharmDr. Ondřej Holas, Ph.D. Consultant: Mgr. Jana Kubačková Student: Lenka Voldřichová Title of thesis: Lipid based nanoparticles: drug delivery platform Lipic nanoparticles, as newly developed dosage forms, can overcome many drawbacks of conventional dosage forms. Their potential can be utilized in particular for prolonged, controlled and targeted release. They can also increase the bioavailability of drugs, especially those with poor solubility and also allow targeting, which causes increased accumulation of lipid nanoparticles in certain tissues compared to other tissues. nanoparticles suitable for drug encapsulation. The particles were prepared by the emulsion evaporation method. Their characterization was performed using a Zetasizer, which measured the particle size and the zeta potential. The properties of the formulations were evaluated in terms of nanoparticle size, polydispersity, zeta potential, and formulation properties. Differencial scanning calorimetry analysis was also performed on selected formulations. The selected final formulation was composed of 25 mg glycerol monostearate, 10 mg isopropyl myristate, 15 mg lecithin and Kolliphor P188 0,1% solution....
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A study of biodegradable polyesters based nanoparticles properties
Blažková, Jiřina ; Holas, Ondřej (advisor) ; Dittrich, Milan (referee)
10 ABSTRACT Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, PhD. Student: Jiřina Blažková Title of thesis: A study of biodegradable polyesters based nanoparticles properties Nanoparticles (NPs) are particles with a diameter size ranging between 1 - 500 nm. They are preferably used as drug delivery systems or imaging systems. NPs are able to encapsulate both hydrophilic and hydrophobic drugs and also macromolecules such as peptides or mRNAs. The aim of this study was to specify selected properties of NPs prepared from poly (lactide-co-glycolide) polymer (PLGA) using polyvinyl alcohol as a surfactant. Nanoprecipitation was chosen as a preparation method. NPs were prepared from a branched PLGA copolymer and from a conventional linear PLGA polymer/oligomer. The main task was a stability study. The effect of the pH and the type of the used polymer of the nanoparticle suspension on the morphology of the nanoparticles was evaluated over one month period. The following parameters of nanoparticles with two model drugs (curcumin and procaine) were also monitored: encapsulation efficiency, drug loading and recovery yield. Dissolution tests were performer and the suitability of individual polymers for different types of drugs...
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Hybrid polymeric-lipid nanoparticles as drug carriers
Žemličková, Simona ; Holas, Ondřej (advisor) ; Smékalová, Monika (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultants: PharmDr. Ondřej Holas, Ph.D. Student: Simona Žemličková Title of thesis: Hybrid polymeric-lipid nanoparticles as drug carriers The work is focused on hybrid polymer-lipid nanoparticles, their advantages obtained from polymer and lipid part, purpose of surface modification, basic properties of nanoparticles, methods of preparation, modification of preparation conditions and use of nanoparticles in medicine. The aim of the experimental part was to prepare nanoparticles composed of polyester and lipid by emulsion evaporation method and nanoprecipitation. Two types of linear polymer poly (lactic-co-glycolic acid) and phosphatidylcholine were used in various ratios. The surfactant used for stabilization was poloxamer Pluronic® F127 and the organic solvents were ethyl acetate and acetone. Curcumin served as a model active substance. The effect of lipid and surfactant on the size and zeta potential of nanoparticles was evaluated. Modification of preparation conditions, which included many process parameters, also influenced the monitored parameters. Encapsulation effectivity and drug loading were also tested. Dissolution tests were performed. It was found that size of nanoparticles...
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Pharmaceutical applications of polyesters as drug nanocarriers
Staňková, Petra ; Holas, Ondřej (advisor) ; Paraskevopoulos, Georgios (referee)
Charles University Faculty of Pharmacy in Hradci Králové Department of Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, PhD. Student: Petra Staňková Title of Thesis: Pharmaceutical applications of polyesters as drug nanocarriers Nanoparticles are nowadays intensively studied and perspective type of a drug carrier. Its potential is based on a possibility of targeted drug delivery and controlled drug release. The theoretical part is about nanoparticles types, polymers derived from α-hydroxyacids (PLA, PGA, PLGA). Focus is given on methods of nanoparticles preparation: dispersion of preformed polymers or the polymerization of monomers. The modification of particles surface and practical use of nanomedicine in healthcare are described in other chapters. The research in experimental part is focused on the influence of different types of PLGA and their weighing on the size, polydispersity, nanoparticles zeta potential and encapsulation efficiency of rhodamine B. Nanoparticles were prepared by nanoprecipitation method or by solvent evaporation method. The Zetasiser ZS 90 device was used to measure the size of the nanoparticles and to measure zeta potential. The result of the research shows the most suitable weighing for creation of nanoparticles is 25 mg. The samples of this weighing show a...
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Evaluation of co-processed excipients containing mannitol or maltodextrins
Chytková, Martina ; Svačinová, Petra (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Petra Svačinová, Ph.D. Student: Martina Chytková Title of Thesis: Evaluation of co-processed excipients containing mannitol or maltodextrins By the co-processing of two or more excipients using the appropriate methods (most often spray drying) are produced substances which are known as co-processed. There are no changes in the chemical structure in their production, the substances interact at the submolecular level. These resulting excipients have better properties than individual components of the mixture. Co-processed excipients are used for the direct compression of tablets and evaluation of their properties can help to choose the suitable material for the formulation. The aim of this thesis is the evaluation of six different co-processed excipients containing mannitol (Parteck® ODT, PROSOLV® ODT, Pharmaburst® , PEARLITOL® Flash) or maltodextrins (GLUCIDEX® 2, GLUCIDEX® 6D). The compressibility (using force- displacement record) and the properties (dimensions, tensile strength, disintegration, friability, pycnometric density and water absorption) of the compressed tablets were evaluated for compression forces of 3 kN, 5 kN and 7 kN. Samples containing maltodextrins showed...
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Formulation of freeze dried tablets for oromucosal administration of peptides
Macáková, Eliška ; Šklubalová, Zdeňka (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: Doc. PharmDr. Zdeňka Šklubalová, Ph.D. Student: Eliška Macáková Title of Thesis: Formulation of freeze dried tablets for oromucosal administration of peptides Freeze-drying is one out of the important methods for stabilization of active substances, particularly peptides, in pharmacy. The formulation of freeze-dried buccal/sublingual tablets for administration of peptides into the oral cavity is the main target of this thesis. The aim is to propose the combination of appropriate excipients and their concentration to achieve the suitable organoleptic properties and disintegration time of the product cake. The measurement of pH, osmolality, the thermal properties of substances, as well as the evaluation of mechanical quality of tablets and their disintegration were used. In conclusion, the combination of excipients for the composition of matrix for the futher development.
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Polymeric pharmaceutical nanoparticles preparation: a process optimization
Bárta, Michal ; Holas, Ondřej (advisor) ; Vraníková, Barbora (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, Ph.D. Student: Michal Bárta Title of Thesis: Preparation of pharmaceutical nanoparticles: optimalization process Pharmaceutical, polymer nanoparticles besides others work as well as a drug carriers. Their uniqueness is not only because of their subcelular size, but as well because of the biodegradability and biocompatibility they hold. The benefit of these nanoparticiples is the possibility of creation of selective naoparticiples which are able to controle long-term release. The formulation of polymer nanoparticles can be reached within methods using preformed polymer or with polymerization of monomers. The main goal of my thesis was to optimize the production process of polymer nanoparticles and the observation of the solvent influences. The methods used for this reaserch were evaporation method and nanoprecipitation. Granulometric and electrical characteristics of particles were measured with Zetasizer ZS 90. Measurements have prooved, that it is preferable to use the nanoparticle method for the prepartion of the the small nanoparticles with low polydispersity and sufficient stability. From the results of the granulometric analysis of nanoparticles made by the...
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Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Houšková, Denisa ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Supervisor: Dr. Georgios Paraskevopoulos, Ph.D. Consultant: Mgr. Anna Nová ková Author: Denisa Houšková Title of thesis: Effect of the generation of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil. Dendrimers can be defined like highly branched, star-shaped macromolecules with nanometer-scale dimensions and unlimited applications in both biological and materials sciences. Polyamidoamine (PAMAM) dendrimers have been used to effectively enhance the (trans)dermal drug delivery of several active substances. Inspired by the structure of PAMAM dendrimers, a new class of dendrimers was designed having amino-functionalized periphery and ethylenediamine core. A repeating motif of bis(2-aminoethyl)glycine was used for generation growth up to the third generation. The new dendritic molecules of zero, first, second and third generation were tested for their ability to enhance the deposition of 5-fluorouracil in the different layers of human skin ex vivo by using Franz diffusion cells. The results suggest that the new dendrimers, at a concentration of 20 mg/mL in 60 % propylene glycol in water as vehicle, are able to deliver 5-fluorouracil at the...
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Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-fluorouracil
Chladová, Pavlína ; Paraskevopoulos, Georgios (advisor) ; Holas, Ondřej (referee)
Effect of the concentration of amino-decorated polyamidoamine dendrimers with ethylenediamine core at the (trans)dermal delivery of 5-Fluorouracil Pavlína Chladová Dendrimers are synthetic, symmetrically tree-like branched molecules. They are composed of repeating units (monomers). They have high density of surface functional groups and spherical shape in solution. Since their molecular weight is highly controllable, they are characterized by monodispersity and this is their main difference from classical polymers. Dendrimers have a wide spectrum of applications in biomedicine. Due to the empty space between the branches of the molecule, they can encapsulate drugs, and by conjugation and complexation to the surface groups, they are able to carry even larger drug molecules. Thus, dendrimers can be used as drug delivery systems. In addition, they have been used for skin application of several active molecules, either as topical or transdermal delivery. Suitable properties for (trans)dermal application have been demonstrated for dendrimers which consist of monomers with amine groups and are connected with amide bonds. The goal of this thesis was the preparation of dendrimers with these characteristics and the evaluation of their concentration influence to the permeability of 5-Fluorouracil (5-FU) to human...
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Process of nanoparticulate systems purification optimization
Strnadová, Kristýna ; Holas, Ondřej (advisor) ; Smékalová, Monika (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, PhD. Student: Kristýna Strnadová Title of thesis: Process of nanoparticulate systems purification optimization The aim of the diploma thesis was to compare three purification methods - centrifugation, size- exclusion chromatography and dialysis, to find the optimal method and its conditions for purification of nanoparticles based on poly(lactic-co-glycolic acid) composed of lactic acid and glycolic acid monomers in a ratio of 50:50. Mentioned purification methods were compared mainly in terms of encapsulation efficiency and recovery yield. Nanoparticles purified by centrifugation were prepared with stabilization of one of the following surfactants: poloxamer 407, poly(vinyl alcohol), cetrimonium bromide (in concentration of 0,1 %, 1 % and 2 %) or sodium cetyl stearyl sulfate (in concentration of 0,01 % and 0,025 %). Purified water and a solution of the stabilizer in the corresponding concentration were used as redispersion media during centrifugation. Centrifugation was performed at 7200 rcf in repeated cycles of 15 min each. Size-exclusion chromatography and dialysis were performed with nanoparticles stabilized with 0,1% poloxamer 407. Silica gel, Sephadex®...
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